AMG 837 calcium hydrate|cas:1259389-38-2|西域试剂

AMG 837 calcium hydrate,98.45%

产品编号：Bellancom-13967B| CAS NO：1259389-38-2| 分子式：C₂₆H₂₁F₃O₃.1/2Ca.H₂O| 分子量：455.45

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-13967B	￥1000.00	杭州北京（现货）
Bellancom-13967B	￥1500.00	杭州北京（现货）
Bellancom-13967B	￥6200.00	杭州北京（现货）
Bellancom-13967B	￥9900.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

AMG 837 calcium hydrate

产品介绍

AMG 837 calcium hydrate 是 GPR40/FFA1 的有效的、具有口服活性的部分激动剂，抑制 [³H]AMG 837 与人类 FFA1 受体的特异性结合， pIC₅₀ 值为 8.13。AMG 837 calcium hydrate 可增强啮齿动物的胰岛素分泌并降低葡萄糖水平。

生物活性

AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [³H]AMG 837 binding at the human FFA1 receptor with a pIC₅₀ of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents.

体外研究

AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC₅₀ of 142±20 nM on islets isolated from mice.
AMG 837 stimulates Ca²⁺ flux with the EC₅₀s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo.
AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats.
AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F = 84%) and a total plasma C_max of 1.4 µM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	8-week old Zucker Fatty Rats
Dosage:	0.03, 0.1, 0.3 mg/kg
Administration:	Oral gavage once daily for 21 days
Result:	Decreased glucose AUC values during the glucose tolerance test (GTT) to 7%, 15%, and 25% at 0.03, 0.1 and 0.3 mg/kg, respectively. Increased insulin levels in the mid- and high-dose groups. Not affected body weights during the 21-day treatment.

Animal Model:	8-week old Sprague-Dawley rats
Dosage:	0.03, 0.1, 0.3 mg/kg
Administration:	A single p.o. administration
Result:	Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	8-week old Zucker Fatty Rats
Dosage:	0.03, 0.1, 0.3 mg/kg
Administration:	Oral gavage once daily for 21 days
Result:	Decreased glucose AUC values during the glucose tolerance test (GTT) to 7%, 15%, and 25% at 0.03, 0.1 and 0.3 mg/kg, respectively. Increased insulin levels in the mid- and high-dose groups. Not affected body weights during the 21-day treatment.

Animal Model:	8-week old Sprague-Dawley rats
Dosage:	0.03, 0.1, 0.3 mg/kg
Administration:	A single p.o. administration
Result:	Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 42 mg/mL (92.22 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1956 mL	10.9782 mL	21.9563 mL
5 mM	0.4391 mL	2.1956 mL	4.3913 mL
10 mM	0.2196 mL	1.0978 mL	2.1956 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (5.49 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.49 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.49 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.49 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。